219331 | β-Catenin/Tcf Inhibitor II, PKF118-310 - Calbiochem

219331
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₇H₇N₅O₂

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      219331-10MG
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      Stocked 
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          Glass bottle 10 mg
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          Description
          OverviewA synthetic cell-permeable actinobacteria pyrimidotriazine-dione that selectively disrupts β-catenin-Tcf4 interaction (IC50 = 0.8 µM in cell-free binding assays) and inhibits β-catenin-regulated cellular transcription activity (IC50 = 0.3 µM in HCT116-based reporter assays). PKF118-310 is demonstrated to reverse β-catenin, but not siamois, mRNA-induced ventral body axis formation in Xenopus embryos, while direct tumor site injection (1 mg/kg/0.5 wk) in HepG2 xenograph mice is shown to increase the number of apoptotic cells and decrease the expression of β-catenin target genes (cyclin D1, c-Myc, survivin) in the tumor mass, resulting in an effective tumor growth retardation (by ~60% after a 4-wk treatment period) in vivo.
          Catalogue Number219331
          Brand Family Calbiochem®
          Synonyms1,6-Dimethylpyrimido[5,6-e][1,2,4]triazine-5,7-dione, Wnt Pathway Inhibitor X
          References
          ReferencesWei, W., et al. 2010. Int. J. Cancer 126, 2426.
          Lepourcelet, M., et al. 2004. Cancer Cell 5, 91.
          Product Information
          FormDark yellow solid
          Hill FormulaC₇H₇N₅O₂
          Chemical formulaC₇H₇N₅O₂
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Purity≥95% by HPLC
          Physicochemical Information
          Dimensions
          Materials Information
          Toxicological Information
          Safety Information according to GHS
          Safety Information
          Product Usage Statements
          Storage and Shipping Information
          Ship Code Ambient Temperature Only
          Toxicity Standard Handling
          Storage +2°C to +8°C
          Protect from Light Protect from light
          Do not freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          219331

          References

          Reference overview
          Wei, W., et al. 2010. Int. J. Cancer 126, 2426.
          Lepourcelet, M., et al. 2004. Cancer Cell 5, 91.
          Data Sheet

          Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

          Revision03-April-2012 JSW
          Synonyms1,6-Dimethylpyrimido[5,6-e][1,2,4]triazine-5,7-dione, Wnt Pathway Inhibitor X
          DescriptionA synthetic cell-permeable actinobacteria pyrimidotriazine-dione that selectively disrupts β-catenin-Tcf4 interaction (IC50 = 0.8 µM in cell-free binding assays) and inhibits β-catenin-regulated cellular transcription activity (IC50 = 0.3 µM in HCT116-based reporter assays). PKF118-310 is demonstrated to reverse β-catenin, but not siamois, mRNA-induced ventral body axis formation in Xenopus embryos, while direct tumor site injection (1 mg/kg/0.5 wk) in HepG2 xenograph mice is shown to increase the number of apoptotic cells and decrease the expression of β-catenin target genes (cyclin D1, c-Myc, survivin) in the tumor mass, resulting in an effective tumor growth retardation (by ~60% after a 4-wk treatment period) in vivo.
          FormDark yellow solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₇H₇N₅O₂
          Structure formulaStructure formula
          Purity≥95% by HPLC
          SolubilityDMSO (100 mg/ml)
          Storage +2°C to +8°C
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesWei, W., et al. 2010. Int. J. Cancer 126, 2426.
          Lepourcelet, M., et al. 2004. Cancer Cell 5, 91.